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Table 1 Single Substrate Assay: Compound IC50 Values (uM)

From: Two additive mechanisms impair the differentiation of 'substrate-selective' p38 inhibitors from classical p38 inhibitors in vitro

Compound

phospho-MK2

phospho-ATF2

substrate selectivity*

SD-0006

0.11 ± 1.2

0.35 ± 1.1

3.3

BIRB 796

7.75 ± 1.3

0.92 ± 1.1

0.12

CMPD1

23.4 ± 1.9

>400**

>17

  1. IC50's are shown ± standard error.
  2. *Substrate Selectivity is defined as a relative measure between inhibiting phospho-ATF2 and phospho-MK2 = (ATF2 IC50)/(MK2 IC50). This quantity is distinct and separable from a compound's potency.
  3. **CMPD1 is unable to completely inhibit phospho-ATF2 within its solubility limits.
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BMC Systems Biology

ISSN: 1752-0509

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